scholarly journals SOLUBILITY AND DISSOLUTION RATE ENHANCEMENT OF EZETIMIBE BY SOLID DISPERSION AND PELLETIZATION TECHNIQUES USING SOLUPLUS AS CARRIER

2019 ◽  
pp. 57-64
Author(s):  
Viswanadh Kunam ◽  
Vidyadhara Suryadevara ◽  
Devala Rao Garikapati ◽  
Venkata Basaveswara Rao Mandava ◽  
RLC Sasidhar
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersion ◽  
Physicochemical Parameters ◽  
Solid Dispersions ◽  
Surface Characteristics ◽  
Sem Analysis ◽  
Angle Of Repose ◽  
In Vitro Dissolution ◽  
Pure Drug

Objective: In the present investigation, an attempt was made to improve the surface characters and solubility of the drug by solid dispersion and coating it on the nonpareil sugar beads as pellets. Methods: Ezetimibe solid dispersions were prepared by kneading method using soluplus. Crospovidone was added as a disintegrant in pellets. Ezetimibe pellets were prepared by dissolving soluplus and crospovidone in ethanol in different ratios and coated on nonpareil sugar beads as a drug layer by pan coating technique. Various physicochemical parameters like particle size, friability, angle of repose and drug content were evaluated for the prepared solid dispersions and pellet formulations. In vitro dissolution studies were carried out in 1% SLS using USP apparatus II. FTIR and SEM analysis were performed for solid dispersions, pellet formulations and its polymers to determine the interactions and surface characteristics. Results: The physicochemical parameters were within the specified I. P limits. It was observed that the solid dispersion formulation ED5 showed better dissolution rate to the extent of 1.07 folds and 1.95 folds when compared to a marketed formulation and the pure drug, respectively. Similarly, pellet formulation EP5 containing 1:5 ratio of ezetimibe to soluplus showed an improved dissolution rate to the extent of 1.173 folds and 2.136 folds when compared to the marketed formulation and the pure drug, respectively. FTIR analysis revealed that there was no major interaction between the drug and the excipients.  Conclusion: From the present study, it was observed that the solubility of ezetimibe was enhanced by soluplus in pellet formulations when compared to solid dispersions.

scholarly journals SOLUBILITY AND DISSOLUTION RATE ENHANCEMENT OF TELMISARTAN BY SOLID DISPERSION AND PELLETIZATION TECHNIQUES USING SOLUPLUS AS CARRIER

2019 ◽  
pp. 50-58
Author(s):  
VISWANADH KUNAM ◽  
DEVALA RAO GARIKAPATI ◽  
VIDYADHARA SURYADEVARA ◽  
VENKATA BASAVESWARA RAO MANDAVA ◽  
RAMESH BABU JANGA ◽  
...  
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersion ◽  
Physicochemical Parameters ◽  
Solid Dispersions ◽  
Angle Of Repose ◽  
In Vitro Dissolution ◽  
Infrared Spectrometry ◽  
Scanning Calorimetry ◽  
Electron Microscopic ◽  
Pure Drug

Objective: In the present investigation, an attempt was made to improve the surface characters and solubility of the drug by solid dispersion and coating it on the nonpareil sugar beads as pellets. Methods: Telmisartan solid dispersions were prepared by kneading method using soluplus. Crospovidone was added as disintegrant in pellets. Telmisartan pellets were prepared by dissolving soluplus and crospovidone in ethanol in different ratios and coated on nonpareil sugar beads as a drug layer by pan coating technique. Various physicochemical parameters like particle size, friability, angle of repose and drug content were evaluated for the prepared solid dispersions and pellet formulations. In vitro dissolution studies were carried out in pH 7.5 phosphate buffer using USP apparatus II. Fourier Transform Infrared Spectrometry, Differential Scanning Calorimetry and Scanning Electron Microscopic analysis were performed for solid dispersions, pellet formulations and its polymers to determine the interactions and surface characteristics. Results: The physicochemical parameters were within the specified I. P limits. It was observed that the solid dispersion formulation TS5 containing 1:5 ratio of telmisartan to soluplus showed better dissolution rate to the extent of 1.143 folds and 2.033 folds when compared to a marketed formulation and the pure drug, respectively. Similarly, pellet formulation TP3 containing 1:3 ratio of telmisartan to soluplus showed an improved dissolution rate to the extent of 1.221 folds and 2.170 folds when compared to the marketed formulation and the pure drug, respectively. FTIR and DSC analysis revealed that there was no major interaction between the drug and the excipients.  Conclusion: From the present study, it was observed that the solubility of telmisartan was enhanced by soluplus in pellet formulations when compared to solid dispersions.

scholarly journals SOLUBILITY AND DISSOLUTION RATE ENHANCEMENT OF EZETIMIBE BY SOLID DISPERSION AND PELLETIZATION TECHNIQUES

2019 ◽  
pp. 407-413
Author(s):  
VISWANADH KUNAM ◽  
VIDYADHARA SURYADEVARA ◽  
DEVALA RAO GARIKAPATI ◽  
VENKATA BASAVESWARA RAO MANDAVA ◽  
SIVA PRASAD SUNKARA
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersion ◽  
Release Kinetics ◽  
Solid Dispersions ◽  
Angle Of Repose ◽  
In Vitro Dissolution ◽  
Infrared Analysis ◽  
Lauryl Sulfate ◽  
Pure Drug

Objective: In the present investigation, an attempt was made to improve the surface characters and solubility of the drug by solid dispersion and coating it on the non-pareil sugar beads as pellets. Methods: Ezetimibe solid dispersions were prepared by solvent evaporation technique using Kollidon VA64 as binder and solubility enhancer. Crospovidone as disintegrant and ethanol was used as solvent. Ezetimibe pellets were prepared by dissolving ezetimibe, kollidonVA64, and crospovidone in ethanol in different ratios and coated on non-pareil sugar beads as a drug layer by pan coating technique. Results: All the formulations were further evaluated for physicochemical parameters such as particle size, friability, angle of repose, and drug content. In vitro dissolution studies were carried out in 1% sodium lauryl sulfate using USP apparatus II. Conclusion: It was observed that the dissolution rate of the solid dispersion formulation ESD5 showed better dissolution rate to the extent of 1.05 folds and 1.824 folds when compared to a marketed formulation and pure drug, respectively. Similarly, formulation EPL5 containing 1:5 ratio of ezetimibe to Kollidon VA64 showed improved dissolution rate to the extent of 1.091 folds and 1.986 folds when compared to the marketed formulation and pure drug, respectively. Majority of the formulations displayed first-order release kinetics and were found to be linear with R2 values in the range of 0.874–0.993. Fourier transform infrared analysis revealed that there was no major interaction between the drug and excipients used in the design of formulation. Scanning electron microscopy analysis was performed for solid dispersions, pellet formulations, and its polymers to determine the surface characteristics.

scholarly journals Enhancement of dissolution rate of Olmesartan medoxomil using urea as carrier by different solid dispersion techniques

2018 ◽  
Vol 1 (1) ◽  
pp. 36-42
Author(s):  
B Sangameswaran ◽  
M Gomathi
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersion ◽  
Solid Dispersions ◽  
Olmesartan Medoxomil ◽  
Angle Of Repose ◽  
In Vitro Dissolution ◽  
Dissolution Profile ◽  
Poor Solubility ◽  
Co Precipitation

The poor solubility of drug substances in water and their low dissolution rate in aqueous G.I.T fluid often leads to insufficient bioavailability. As per Biopharmaceutical Classification System (BCS), Olmesartan belongs to the class-II category having poor solubility and high permeability. Since only dissolved drug can pass the gastrointestinal membrane, the proper solubility of the drug is ultimately desired. Its oral bioavailability is 26%. Hence, an attempt was made to enhance its solubility by formulating solid dispersions using different techniques viz., Melting, Kneading, Co-precipitation, Solvent evaporation and Physical mixing etc., Drug and carrier (Urea) in different ratios like 1: 1, 1: 2, 1: 3 and 1:4 were used for formulating solid dispersions. The compatibility of the drug with the carrier was checked by FTIR studies, these results revealed that there was no interaction between them. The angle of repose, bulk density, tapped density; Carr’s index and Hausner ratio were calculated for the micrometric characterization of all the solid dispersions. The drug content was found to be high and uniform in all formulations. The prepared Solid dispersion SEM4 (1:4) showed minimal wetting time of 13 seconds compared with the other formulations. In vitro dissolution, release studies in Phosphate buffer pH of 6.8 revealed that the prepared solid dispersions showed faster drug release compared with the pure drug.  The in vitro dissolution profile showed ascendency on increasing the carrier concentration

scholarly journals Enrichment of aqueous solubility and dissolution profile of mesalamine: In vitro evaluation of solid dispersion

2021 ◽  
Vol 9 (2) ◽  
pp. 127-135
Author(s):  
Anil Raosaheb Pawar ◽  
Pralhad Vitthalrao Mundhe ◽  
Vinayak Kashinath Deshmukh ◽  
Ramdas Bhanudas Pandhare ◽  
Tanaji Dilip Nandgude
Keyword(s):  
Ulcerative Colitis ◽  
Drug Release ◽  
Dissolution Rate ◽  
Solid Dispersion ◽  
Solid Dispersions ◽  
Aqueous Solubility ◽  
In Vitro Dissolution ◽  
Dissolution Profile ◽  
Peg 4000

The aim of the present study was to formulate solid dispersion (SD) of Mesalamine to enrich the aqueous solubility and dissolution rate. Mesalamine is used in the management of acute ulcerative colitis and for the prevention of relapse of active ulcerative colitis. In the present study, Solid dispersion of Mesalamine was prepared by Fusion and Solvent evaporation method with different polymers. SD’s were characterized by % practical yield, drug content, Solubility, FT-IR, PXRD (Powder X- ray diffractometry), SEM (Scanning electron microscopy), in vitro dissolution studies and Stability studies. The percent drug release of prepared solid dispersion of Mesalamine by fusion and solid dispersion method (FM47, FM67, SE47 and SE67) in 1:7 ratio was found 81.36±0.41, 86.29±0.64, 82.45±0.57and 87.25±1.14 respectively. The aqueous solubility and percent drug release of solid dispersion of Mesalamine by both methods was significantly increased. The PXRD demonstrated that there was a significant decrease in crystallinity of pure drug present in the solid dispersions, which resulted in an increased aqueous solubility and dissolution rate of Mesalamine.The significant increase in aqueous solubility and dissolution rate of Mesalamine was observed in solid dispersion as the crystallinity of the drug decreased, absence of aggregation and agglomeration, increased wetability and good dispersibility after addition of PEG 4000 and PEG 6000.

scholarly journals DEVELOPMENT AND IN VITRO DISSOLUTION STUDY OF BINARY AND TERNARY SOLID DISPERSIONS OF ACECLOFENAC

2019 ◽  
Author(s):  
Md. Shahidul Islam ◽  
Rasheda Akter Lucky
Keyword(s):  
Polyethylene Glycol ◽  
Dissolution Rate ◽  
Solid Dispersion ◽  
Drug Carrier ◽  
Solid Dispersions ◽  
Weight Ratio ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
Peg 6000

The poor aqueous solubility of the drug exhibits in variable dissolution rate and hence poor bioavailability. Aceclofenac is poorly water soluble drug. The aim of the present study was to improve the water solubility and the dissolution rate of Aceclofenac by solid dispersion technique using different water soluble polymers. The term solid dispersions refer to the dispersions of one or more active ingredients in an inert carrier or matrix at solid state. In this study, binary solid dispersion of Aceclofenac were prepared by fusion method using Polyethylene glycol 6000 (PEG 6000), Polyethylene glycol 4000 (PEG 4000), Poloxamer as carrier. Different drug-carrier weight ratio was used for this study. The effect of the carrier on the solubility and in-vitro dissolution were studied. It was found the drug was released 26.86% after 5 minutes and only 40.19% within 60 mins from active Aceclofenac on the other hand the release pattern of Aceclofenac from the binary SD formulation containing PEG 6000 in 1:5 ratio (Formulation coding: A5) showed the best result in comparison of other binary and ternary SD formulations which was 62.29% after 5 min and 83.03% within 60 mins. The hydrophilic polymers used for the preparation of solid dispersion are showed significant increase in the solubility of Aceclofenac.

scholarly journals Effect of Amphiphilic Graft Co-Polymer Carrier on Solubility and Dissolution Enhancement of Ambrisentan

2021 ◽  
pp. 329-338
Author(s):  
Rahul Radke ◽  
Neetesh K. Jain
Keyword(s):  
Ftir Spectroscopy ◽  
Dissolution Rate ◽  
Solid Dispersion ◽  
Solid Dispersions ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
Dissolution Enhancement ◽  
Polymer Carrier ◽  
Dissolution Study

Aim: Ambrisentan is a endothelin type A selective receptor antagonist used in the management of pulmonary arterial hypertension. Ambrisentan is BCS Class II drug haves very poor solubility in water and shows incomplete absorption after oral administration. The present work was aimed to study the effect of amphiphilic graft co-polymer carrier on enhancement of solubility and dissolution rate of poorly water soluble drug ambrisentan. To improve the aqueous solubility of ambrisentan solid dispersion was formulated by using novel carrier amphiphilic graft co-polymer (Soluplus® ). Materials and Methods: Solid dispersion was prepared by kneading technique by utilizing various ratios of carrier. Obtained solid dispersions ware evaluated for solubility, percentage yield, drug content and in vitro dissolution study. Powder characterization was performed by infrared (FTIR) spectroscopy, differential scanning calorimetry (DSC), and X-ray diffraction (XRD). Results: FTIR spectroscopy shows no interaction between drug and polymer. DSC study showed that endothermic peak of drug was completely disappeared in Solid dispersion suggesting complete miscibility of drug in Soluplus®. XRD study suggest the conversion of crystalline ambrisentan in to amorphous form. All solid dispersions prepared with Soluplus® as a carrier showed increase in solubility. Solubility of ambrisentan was found to be increased 7.17 fold in optimized SD formulation ASD5. In vitro dissolution study showed the faster drug release from SD formulation compare to its pure form. All solid dispersion formulation’s release more than 50% of drug in first 10 min. Conclusion: This study conclude that the preparation of amphiphilic graft co-polymer based solid dispersion prepared by kneading technique is found to be useful in enhancement the solubility and dissolution rate of ambrisentan.

ENHANCEMENT OF ORAL BIOAVAILABILITY AND DISSOLUTION RATE OF ACECLOFENAC USING SOLID DISPERSIONS BY DROPPING METHOD

INDIAN DRUGS ◽  
2012 ◽  
Vol 49 (12) ◽  
pp. 36-43
Author(s):  
B. V Reddy ◽  
◽  
J Venkata Raju ◽  
M Jalaiah ◽  
Nageswara Rao ◽  
...  
Keyword(s):  
Dissolution Rate ◽  
Oral Bioavailability ◽  
Release Kinetics ◽  
Solid Dispersions ◽  
In Vitro Dissolution ◽  
Peg 6000 ◽  
Saturation Solubility ◽  
Pure Drug ◽  
Physical Mixtures

In the present study, the aim was to enhance the oral bioavailability and dissolution rate of aceclofenac by solid dispersions using polyethylene glycol (PEG-6000) as a carrier and to study the effect of carrier on dissolution rate. Initial studies were carried out using physical mixtures of the drug and carrier. Solid dispersions were prepared by fusion technique using dropping method. Aceclofenac was formulated as physical mixtures and solid dispersions (dropping method) using 1:2, 1:4, 1:6 and 1:8 ratios of drug and carrier (PEG 6000). Saturation solubility study for pure drug, physical mixtures and solid dispersions were carried out in water and pH 6.8 phosphate buffer solutions (PBS). The In vitro dissolution studies were carried in pH 6.8, higher in vitro dissolution of solid dispersions was recorded compared to their corresponding physical mixtures and the pure drug. The prepared solid dispersions were observed that increased in the saturation solubility and dissolution rate of aceclofenac than that of pure drug. PEG 6000 in 1: 8 drug to carrier ratio exhibited the highest drug release (98.69%) formulated as solid dispersions using dropping method. The FT-IR study shows that drug was stable in solid dispersions and there were no interactions. It is concluded that dissolution rate was improved by solid dispersion of aceclofenac: PEG6000 prepared as 1:8 ratio by dropping method showed excellent physicochemical characteristics and was found to be described by dissolution release kinetics and was selected as the best formulation.

DEVELOPMENT OF SOLID DISPERSION TABLET OF CARVEDILOL TO IMPROVE SOLUBILITY

INDIAN DRUGS ◽  
2016 ◽  
Vol 53 (01) ◽  
pp. 54-59
Author(s):  
S. S Shelake ◽  
◽  
R. G Gaikwad ◽  
S Patil ◽  
F. I. Mevekari ◽  
...  
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersion ◽  
Solid Dispersions ◽  
Aqueous Media ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
Scanning Calorimetry ◽  
Water Soluble Drugs ◽  
Ft Ir

Crystalline state compounds are typically dissolution rate limited and dissolution rate is directly proportional to the solubility for BCS class II or class IV compounds. Solid dispersions are one of the most promising strategies to improve the oral bioavailability poorly water soluble drugs. The purpose of this study was to increase solubility of carvedilol by solid dispersion (SDs) technique with Poloxamer (PXM) 407 in aqueous media. The carvedilol- PXM 407 solid dispersion was prepared by solvent evaporation, kneading and melting method. It was characterized by differential scanning calorimetry (DSC), X-ray powder diffraction (XRD), Fourier transformation infra-red spectroscopy (FT-IR), scanning electron microscopy (SEM) and in vitro dissolution studies. The prepared solid dispersion were found to have higher dissolution rates as compared to intact carvedilol. During formulation of solid dispersion crystalline to amorphous transition has been observed.

scholarly journals FORMULATION DEVELOPMENT AND CHARACTERISATION OF MECLIZINE HYDROCHLORIDE FAST DISSOLVING TABLETS USING SOLID DISPERSION TECHNIQUE

2018 ◽  
Vol 10 (4) ◽  
pp. 141 ◽  
Author(s):  
Prashant Bhide ◽  
Reeshwa Nachinolkar
Keyword(s):  
Drug Release ◽  
Solid Dispersion ◽  
Phosphate Buffer ◽  
Solid Dispersions ◽  
In Vitro Dissolution ◽  
Formulation Development ◽  
In Vitro Drug Release ◽  
Drug Content ◽  
Pure Drug

Objective: The aim of the present investigation was to design and evaluate fast dissolving tablet (FDT) for the oral delivery containing solid dispersion of meclizine (MCZ) hydrochloride, an antiemetic drug.Methods: The solubility of meclizine was increased by preparing solid dispersions using mannitol as a carrier by fusion method. The prepared solid dispersion, was subjected for in vitro drug release, percent practical yield, drug content, infrared spectroscopy (IR), differential scanning calorimetry (DSC), scanning electron microscopy (SEM). Optimized solid dispersion was incorporated to prepare fast dissolving tablets. Preformulation studies were carried out on tablet blends. The prepared solid dispersion, as well as pure drug fast dissolving tablets, was evaluated for drug content, weight variation, hardness, friability, in vitro drug release, wetting time, disintegration time, water absorption ratio, in vitro dispersion time.Results: Meclizine pure drug, solid dispersions formulations SD1, SD3 and SD5 showed 12.8, 31.68, 38.92 and 53.28% cumulative drug release in phosphate buffer pH 6.8 after 60 min, respectively. Thus faster dissolution rate was exhibited by the solid dispersion containing 1:5 (w/w) ratio of meclizine: mannitol. Percent cumulative drug release for control and solid dispersion tablets after 60 min in phosphate buffer pH 6.8 was 92.04 and 98.2% respectively. The release of drug meclizine from best formulation SD5 FDT was found to be faster than pure drug FDT.Conclusion: Fast dissolving tablet of optimized solid dispersion showed better in vitro dissolution result then FDT of pure drug at the end of one hour.

scholarly journals FORMULATION AND EVALUATION OF TELMISARTAN SOLID DISPERSIONS USING ENTADA SCANDENS SEED STARCH AND POLOXAMER-188 AS SUPERDISINTEGRANTS

2018 ◽  
Vol 11 (9) ◽  
pp. 474
Author(s):  
Venkatarao Mannem ◽  
Vidyadhara Suryadevara ◽  
Sandeep Doppalapudi
Keyword(s):  
Physicochemical Properties ◽  
Sodium Hydroxide ◽  
Dissolution Rate ◽  
Solid Dispersion ◽  
Solid Dispersions ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
Differential Scanning Calorimetric ◽  
Poloxamer 188

Objective: The current research focuses on solubility enhancement of poorly water-soluble drug telmisartan, using novel superdisintegrants such as Entada scandens seed starch and Poloxamer-188. Starches yielded from plants are pharmaceutically useful as binders, diluents, disintegrants, and lubricants.Methods: Starches were extracted from E. scandens seed powder using alkali method (sodium hydroxide at 0.1%, 0.25%, and 0.5% concentrations) and water. These starches were subjected for the evaluation of various physicochemical properties and phytochemical tests.Results: The phytochemical tests revealed the presence of only starch in all the extracts. Of all the starches, the starch prepared from 0.5% sodium hydroxide (ESS4) showed best physicochemical properties. Solid dispersions were prepared using telmisartan, poloxamer-188, and starch (ESS4) in various concentrations using fusion technique. Various pre-formulation parameters were evaluated. From in vitro dissolution studies, it was observed that the solid dispersion formulation TP7 containing telmisartan and poloxamer-188 in 1:4 ratios showed better dissolution rate. Solid dispersion TPS7 containing TP7 formulation and 15% w/w of alkali extracted starch showed faster disintegration and enhanced dissolution rate than the solid dispersions prepared alone with poloxamer-188. Fourier transform infrared spectroscopy and differential scanning calorimetric studies for optimized formulations revealed that there were no major interactions between the drug and excipients. X-ray diffraction studies revealed the crystalline and amorphous nature of formulations.Conclusion: Thus, the solid dispersions prepared using E. scandens seed starch revealed the superdisintegrant property of starch. 

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